Cat. No. | Product name | CAS No. |
DC8020 |
A77-01
Featured
A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. |
607737-87-1 |
DC11778 |
PKC-IN-6c
A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM). |
2026603-86-9 |
DC7286 |
A83-01
Featured
A83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). |
909910-43-6 |
DC10052 |
Bisindolylmaleimide X(Ro 31-8425)
Featured
Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC). |
1241725-89-2 |
DC8504 |
Bisindolylmaleimide X HCl
Featured
Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC). |
145317-11-9 |
DC11038 |
Bryostatin 1
Featured
Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM). |
83314-01-6 |
DC7643 |
DMH1
Featured
DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. |
1206711-16-1 |
DC5057 |
Enzastaurin (LY317615)
Featured
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
170364-57-5 |
DC8342 |
EW-7197
Featured
EW-7197 is a potent ALK5 inhibitor. EW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy. |
1352608-82-2 |
DC7132 |
GF 109203X
Featured
GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
133052-90-1 |
DC7660 |
Go 6983
Featured
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ. |
133053-19-7 |
DC7980 |
GW-6604
Featured
GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity. |
452342-37-9 |
DC7146 |
GW788388
Featured
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor. |
452342-67-5 |
DC7835 |
H-89 2HCl
Featured
H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
130964-39-5 |
DC10983 |
ICA-1(ICA-1T)
Featured
ICA-1(ICA-1T)is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member. |
742038-81-9 |
DC8028 |
ITD-1
Featured
ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells. |
1099644-42-4 |
DC7742 |
K02288
Featured
K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA. |
1431985-92-0 |
DC7914 |
LDN-214117
Featured
LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM). |
1627503-67-6 |
DC7189 |
LY-2109761
LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2. |
700874-71-1 |
DC6306 |
LY2157299(Galunisertib)
Featured
LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2. |
700874-72-2 |
DC10675 |
LY3200882
Featured
LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor. |
1898283-02-7 |
DC8523 |
LY333531 Hydrochloride(Ruboxistaurin HCl)
Featured
LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). It is potentially beneficial for cancer research. |
169939-93-9 |
DC7587 |
ML347
Featured
ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM |
1062368-49-3 |
DC10645 |
Phorbol 12-myristate 13-acetate (PMA)
Featured
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM. |
16561-29-8 |
DC7634 |
PKC-412 (Midostaurin)
Featured
PKC-412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. |
120685-11-2 |
DC8022 |
R-268712
Featured
Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler |
879487-87-3 |
DC7259 |
Repsox(ALK5 Inhibitor II)
Featured
RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively. |
446859-33-2 |
DC7270 |
Ro 31-8220 mesylate
Featured
Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively. |
138489-18-6 |
DC5189 |
SB-431542
Featured
SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases. |
301836-41-9 |
DC6312 |
SB525334
Featured
SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. |
356559-20-1 |
DC7739 |
SD-208
Featured
SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM) |
627536-09-8 |
DC7506 |
Sotrastaurin
Featured
Sotrastaurin(AEB-071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ. |
425637-18-9 |
DC9698 |
Staurosporine
Featured
Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively. |
62996-74-1 |
DC12308 |
VTX-27
Featured
VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ. |
1321924-70-2 |
DC10984 |
ζ-Stat (ZETA-STAT)
Featured
ζ(ZETA)-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13% inhibition on PKC-I at 20 uM. |
3316-02-7 |
DC7421 |
GO 6976
Featured
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3. |
136194-77-9 |
DC7382 |
CGP60474
Featured
CGP60474 is a potent inhibitor of cyclin-dependent kinase (CDK). |
164658-13-3 |
DC28223 |
Bisindolylmaleimide IV
Featured
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM. |
119139-23-0 |
DC28454 |
PS315
PS315, a derivative of PS48, is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCι (IC50=30 μM). PS315 has anti-cancer activity. |
1221964-50-6 |
DC28544 |
N-Desmethyltamoxifen
Featured
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. |
31750-48-8 |
DC28545 |
N-Desmethyltamoxifen hydrochloride
Featured
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent re |
15917-65-4 |
DC28553 |
TGFBR1-IN-1
TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM. |
2170830-26-7 |
DC29096 |
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier. |
|
DC31048 |
PKCiota-IN-51
PKCiota-IN-51 is a potent and selective inhibitor of Protein Kinase C iota (PKC-ι) with IC50 of 2.7 nM, >15-fold selectivity over PKC-α and PKC-β. |
|
DC31061 |
JL5
JL5 is a novel potent, selective BMP receptor inhibitor with IC50 of 1, <5 and 2 nM for ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B, respectively. |
2244238-50-2 |
DC39110 |
TGF-beta/Smad inhibitor
The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody. |
|
DC40063 |
Delcasertib hydrochloride
Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI). |
|
DC40105 |
Ro 32-0432 hydrochloride
Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research. |
1781828-85-0 |
DC40325 |
ζ-Stat trisodium
Featured
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro. |
31894-34-5 |
DC40357 |
PKC-iota inhibitor 1
Featured
PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM. |
2328094-11-5 |
DC41012 |
ALK2-IN-4
Featured
ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base. |
2248154-85-8 |
DC41013 |
ALK2-IN-4 succinate
ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base. |
2416307-25-8 |
DC41031 |
Ingenol 3,20-dibenzoate
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells. |
59086-90-7 |
DC41338 |
Isosaponarin
Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin increases collagen synthesis, caused by up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production. |
19416-87-6 |
DC41499 |
Disitertide TFA
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer. |
|
DC41721 |
ZIP
ZIP is a selective peptide inhibitor of PKMζ. ZIP injections can block the impairment in morphine conditioned place preference induced. |
863987-12-6 |
DC41722 |
ZIP TFA
ZIP TFA is a selective peptide inhibitor of PKMζ. ZIP TFA injections can block the impairment in morphine conditioned place preference induced. |
|
DC41723 |
PKC β pseudosubstrate
PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC. |
172308-76-8 |
DC41724 |
PKC β pseudosubstrate TFA
PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC. |
|
DC41725 |
[Ala113]MBP(104-118)
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM. |
99026-78-5 |
DC41726 |
[Ala107]MBP(104-118)
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM. |
99026-77-4 |
DC41727 |
[Ala107]MBP(104-118) TFA
[Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM. |
|
DC41728 |
[Ala113]MBP(104-118) TFA
[Ala113]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM. |
|
DC41892 |
pm26TGF-β1 peptide
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction. |
|
DC41893 |
pm26TGF-β1 peptide TFA
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction. |
|
DC42550 |
Pep2m, myristoylated
Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. |
1423381-07-0 |
DC43997 |
Epsilon-V1-2
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC. |
182683-50-7 |
DC44218 |
HBDDE
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis. |
154675-18-0 |
DC45279 |
LSKL, Inhibitor of Thrombospondin (TSP-1)
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier. |
283609-79-0 |
DC45690 |
Ruboxistaurin
Ruboxistaurin (LY333531) is an orally active, selective PKCβ inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKCβI with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKCβII with an IC50 of 5.9 nM. |
169939-94-0 |
DC45825 |
1-Stearoyl-2-arachidonoyl-sn-glycerol
1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity. |
65914-84-3 |
DC45863 |
Leucosceptoside A
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitory activity against α-glucosidase and PKCα (IC50 of 19.0 μM). |
83529-62-8 |
DC46247 |
TGFβRI-IN-1
TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively . |
1950628-94-0 |
DC46417 |
TGFβRI-IN-3
Featured
TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology. |
2763602-67-9 |
DC46451 |
CC-90005
Featured
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression. |
1799574-70-1 |
DC46505 |
Mezerein
Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC. |
34807-41-5 |
DC46926 |
Bisindolylmaleimide XI hydrochloride
Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively. |
145333-02-4 |
DC46927 |
PF-03622905
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases. |
1072100-15-2 |
DC46989 |
Myelin Basic Protein TFA
Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts. |
|
DC47156 |
Sangivamycin
Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers. |
18417-89-5 |
DC47189 |
Bryostatin 3
Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion. |
143370-84-7 |
DC47209 |
PF-04577806
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats. |
1072100-81-2 |
DC47378 |
(±)-1,2-Diolein
(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. |
2442-61-7 |
DC47379 |
1,2-Didecanoylglycerol
1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC). |
17863-69-3 |
DC48356 |
1-Oleoyl-2-acetyl-sn-glycerol
1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production. |
86390-77-4 |
DC48425 |
TGFβR-IN-1
TGFβR-IN-1 is a long-acting tumor-activated prodrug of a TGFβR inhibitor. |
|
DC48741 |
TGFβ-IN-1
TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway. |
883560-84-7 |
DC49041 |
Teleocidin A1
Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM). |
70497-14-2 |
DC50084 |
Mongersen
Mongersen is a 21-mer phosphorothioate antisense oligonucleotide targeting the mRNA of the Smad7 protein, thus leading to suppression of TGF-β1 pathways and remission of Crohn's disease. |
1443994-46-4 |
DC50085 |
SC-9
SC-9 is a PKC activator in the presence of Ca2+. |
102649-78-5 |
DC50086 |
Safingol
Safingol is a lyso-sphingolipid PKC (protein kinase C ) inhibitor. |
15639-50-6 |
DC50087 |
1,2-Dimyristoyl-sn-glycerol
Featured
1,2-Dimyristoyl-sn-glycerol is a saturated diacylglycerol and a weak second messenger for the activation of PKC. |
60562-16-5 |
DC50088 |
H-7 inhibitor
Featured
H-7 is a specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol. |
84477-87-2 |
DC50281 |
Chromenone 1
Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs. |
1639929-29-5 |
DC50283 |
ALK5-IN-9
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease. |
2489611-06-3 |
DC50284 |
ALK5-IN-8
ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1). |
2705900-81-6 |
DC50285 |
Myostatin-IN-1
Myostatin-IN-1 is a potent myostatin inhibitor (IC50 of 0.19, 0.63, 0.89 and 1.6 μM for myostatin, GDF-11, activin A and TGF-β1, respectively). Myostatin-IN-1 increases the tibialis anterior muscle mass in mice. Myostatin-IN-1 can be used for researching the prolonged inactivation of myostatin in skeletal muscle. |
2757831-08-4 |
DC70659 |
NP627
NP627 (NP-627) is a specific small-molecule inhibitor of protein kinase C deltaI (PKCδI) with Kd of 1 nM.NP627 inhibits the cleavage of PKCδI in adipocyte (at 10 nM) and decreases PKCδI kinase activity.NP627 does not inhibit other PKC isozyme activities.NP627 prevents caspase-3 mediated cleavage of PKCδI, significantly inhibits PKCδI catalytic fragment release, decreases inflammation and apoptosis, and significantly improves mitochondrial metabolism in human adipocytes from obese individuals. |
412962-32-4 |
DC70688 |
PF-06952229
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor, specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction, shows with potential antineoplastic activity. |
1801333-55-0 |
DC70699 |
PKCθ inhibitor 22
PKCθ inhibitor 22 is a potent, selective, orally bioavailable inhibitor of Protein Kinase Cθ (PKCθ) with IC50 of 6 nM.PKCθ inhibitor 22 inhibits IL-2 release from PBMCs following stimulation with anti-CD3/CD28 (IC50=0.19 uM).PKCθ inhibitor 22 also inhibits the release of IL-17 from CD3/CD28 stimulated Th-17 cells with an IC50 of 1 uM.PKCθ inhibitor 22 demonstrated a reduction of symptoms in a mouse model of multiple sclerosis. |
1160501-81-4 |
DC71011 |
Bisindolylmaleimide II
Bisindolylmaleimide II is a general inhibitor of all PKC subtypes. |
137592-45-1 |
DC71128 |
TP0427736 hydrochloride
TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA). |
2459963-17-6 |
DC71622 |
pm26TGF-β1 peptide (TFA)
Pm26TGF-β1 peptide TFA is a peptide is a portion of the human TGF-β1 molecule, which shows high affinity for the TGF-β1 receptor. |
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DC71913 |
SJ000063181
SJ000063181 is a potent BMP signaling activator with an EC50 ≤1 µM. SJ000063181 can be used as chemical probes to interrogate BMP signaling due to it can penetrate zebrafish embryos. |
945189-68-4 |
DC71914 |
SY-LB-35
SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways. |
2603461-70-5 |
DC72005 |
SY-LB-57
SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension. |
2253719-35-4 |
DC72746 |
7-Oxostaurosporine
7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway. |
125035-83-8 |
DC74370 |
Z640
Z640 is a novel non-selective atypical PKC (aPKC) agonist, increases PKCζ and PKCι kinase activity with EC50 of 1.09 and 3.47 µM in vitro kinase activity assays, respectively. |
353793-07-4 |
DC74371 |
CDD-1115
CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM. |
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DC74372 |
CDD-1281
CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM. |
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DC74373 |
CDD-1653
CDD-1653 (CDD1653) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 2.8 nM, >360-fold over ALK1, and is inactive versus all other type 1 and type 2 TGFβ family kinases. |
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DC74374 |
Ki26894
Ki26894 (Ki 26894) is a small molecule TGF-beta type I receptor (TbetaR-I) kinase inhibitor, inhibits TGF-β-induced transcriptional activation in MDA-231-D-TβFluc/Rluc cells with IC50 of 0.49 uM. |
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DC74375 |
SRI-31277
SRI-31277 is a tripeptide inhibitor of thrombospondin 1 activation of TGF-β, specifically inhibits TGF-β activation mediated through TSP-1 with pIC50 of 8.28 nM. |
1637468-93-9 |